- 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE
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The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, e
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Page/Page column 198
(2015/03/28)
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- BICYCLIC PYRROLE DERIVATIVES USEFUL AS AGONISTS OF GPR120
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The present invention is directed to bicyclic pyrrole derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example. Type II diabetes mellitus.
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Page/Page column 90
(2015/09/28)
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- BICYCLIC PYRROLE DERIVATIVES USEFUL AS AGONISTS OF GPR120
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The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
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Paragraph 0374; 0375
(2014/09/30)
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- Bicyclic pyrrole derivatives useful as agonists of GPR120
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The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
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Page/Page column 74
(2015/01/06)
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- CONDENSED TRICLYCLIC COMPOUNDS AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted -(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inbitor of HIV replication.
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Page/Page column 93
(2013/07/05)
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- UREA INHIBITORS OF MAP KINASES
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Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.
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Page/Page column 26
(2010/03/04)
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- A simple Cu-catalyzed coupling approach to substituted 3-pyridinol and 5-pyrimidinol antioxidants
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(Chemical Equation Presented) A convenient approach to 3-pyridinols and 5-pyrimidinols via a two-step Cu-catalyzed benzyloxylation/catalytic hydrogenation sequence is presented. The corresponding 3-pyridinamines and 5-pyrimidinamines can be prepared in an analogous sequence utilizing benzylamine in lieu of benzyl alcohol. The radical-scavenging ability of these derivatives are preliminarily explored and reveal that the increased acidities of the pyridinols and pyrimidinols render them susceptible to more significant kinetic solvent effects when compared to phenols.
- Nara, Susheel J.,Jha, Mukund,Brinkhorst, Johan,Zemanek, Tony J.,Pratt, Derek A.
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supporting information; experimental part
p. 9326 - 9333
(2009/04/06)
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- COMPOUNDS
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The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
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Page/Page column 23
(2010/02/15)
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- Triazole antifungal agents
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PCT No. PCT/EP96/02470 Sec. 371 Date Dec. 19, 1997 Sec. 102(e) Date Dec. 19, 1997 PCT Filed Jun. 5, 1996 PCT Pub. No. WO97/01552 PCT Pub. Date Jan. 16, 1997The invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein Ar, Z and Het are as defined herein. The compounds of formula (I) possess activity as antifungal agents. The invention also relates to pharmaceutical compositions containing said compounds of formula (I) and to methods of treating fungal infections by administering said compounds of formula (I).
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- Triazole antifungal agents
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An antifungal compound of formula (I): STR1 or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl substituted with 1 to 3 substituents each independently selected from halo and CF3 ; R2 is (hydroxy)C1 -C4 alkyl, CONH2, S(O)m (C1 -C4 alkyl), Ar or Het; m is 1 or 2; Ar is phenyl optionally monosubstituted with halo or CF3 ; and Het is a C-linked 6-membered nitrogen-containing aromatic heterocyclic group containing 1 or 2 nitrogen atoms, or a C- or N-linked 5-membered nitrogen-containing aromatic heterocyclic group containing from 2 to 4 nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C1 -C4 alkyl or (C1 -C4 alkoxy)methyl.
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- Substituted pyridines as selective cyclooxygenase-2 inhibitors
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The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
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- Triazole antifungal agents
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The invention provides antifungal compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by up to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1
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- A Convenient Palladium-Catalyzed Coupling Approach to 2,5-Disubstituted Pyridines
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2,5-Dibromopyridine has been found to undergo a regioselective palladium-catalyzed coupling reaction with terminal acetylenes and arylzinc halides to give the corresponding 2-alkynyl-5-bromo- and 2-aryl-5-bromopyridines, respectively, in 70percent-90percent isolated yields.To complement this chemistry, the triflate derived from 2-methyl-5-pyridinol was found to participate in a palladium-catalyzed reaction with terminal acetylenes leading to the corresponding 5-alkynyl-2-methylpyridines.These intermediates can be further manipulated to afford a broad range of 2,5-disubstituted pyridines.
- Tilley, Jefferson W.,Zawoiski, Sonja
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p. 386 - 390
(2007/10/02)
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